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Compound Detail

CHEMBL5418159

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O=c1cc(-c2ccc(O)c(O)c2)oc2cc(F)cc(O)c12

Basic Information

ChEMBL ID CHEMBL5418159
Phase Preclinical
Structure Type MOL
InChI Key QEXKRCJFEQQDDO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

288.2
MW (Da)
2.72
ALogP
5
HBA
3
HBD
90.9
PSA (Ų)
0.60
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H9FO5
MW 288.23
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness 0.88

Activity Summary

IC50 1 meas. best 4.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA polymerase eta
CHEMBL5542
IC50 4.86 4.86 13800.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.0 hr Mus musculus
T1/2 1.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
DNA polymerase eta IC50 = 13800.0 nM 4.86 Inhibition of C-terminal 6xHis-tagged human DNA polymerase eta (1 to 511 residue... 36621139

Literature References

PubMed DOI Target Context # Activities
36621139 10.1016/j.ejmech.2022.115044 ADMET 2
36621139 10.1016/j.ejmech.2022.115044 DNA polymerase eta 1
36621139 10.1016/j.ejmech.2022.115044 No relevant target 1

Data from ChEMBL 36 via Core Engine